79534-96-6

Upstream product

• 66762-68-3 ethyl 4-methoxy-3-oxobutanoate 

Downstream Products

• 55551-60-5 2-methoxymethyl-4-(3'-nitrophenyl)-1,4-dihydropyridine-3,5,6-tricarboxylic acid triethyl ester 
• 817553-57-4 6-(4-chlorophenyl)-5-(2,4-dichlorophenyl)-2-methoxymethylpyridine-3-carboxylic acid ethyl ester 
• 140171-81-9 2-(2-Amino-ethoxymethyl)-4-(2-chloro-phenyl)-6-methoxymethyl-1,4-dihydro-pyridine-3,5-dicarboxylic acid diethyl ester 
• 140171-55-7 4-(2-Chloro-phenyl)-2-[2-(1,3-dioxo-1,3-dihydro-isoindol-2-yl)-ethoxymethyl]-6-methoxymethyl-1,4-dihydro-pyridine-3,5-dicarboxylic acid diethyl ester 

Relevant academic research and scientific papers

DIPHENYLPYRIDINE DERIVATIVES, PREPARATION AND THERAPEUTIC APPLICATION THEREOF

The invention relates to 5,6-diphenylpyridine-3-carboxamide derivatives of general formula (I): where: R1 represents hydrogen or a (C1-C 4)alkyl; R2 represents: a monoazo saturated heterocycle of 5 to 7 atoms, the nitrogen atom being substituted with a (C1-C4)alkanoyl; NR10R11; a nonaromatic (C3-C10) carbocycle more than tri-substituted with (C1-C4)alkyl; a nonaromatic (C11-C12) carbocycle unsubstituted or mono-or polysubstituted with (C1-C4) alkyl; a monooxygenated saturated heterocycle with 5 to 7 atoms, more than tri-substituted with (C1-C4)alkyl; or R1 and R2, together with the nitrogen atom to which the above are bonded, form a 4-disubstituted piperidin- 1-yl group; the salts, solvates and hydrates thereof. The invention further relates to a method for production and therapeutic application thereof.

Long-acting dihydropyridine calcium antagonists. 9. Structure activity relationships around amlodipine

The preparation of a range of 1,4-dihydropyridine analogues of amlodipine has been undertaken and their calcium antagonist activities on rat aorta have been evaluated.Increasing the size of the C5 ester group dramatically reduces calcium antagonist activity, a trend which would be compatible with the carbonyl group of that ester binding to the DHP receptor.Amlodipine analogues with extended C3 ester substituents also have lower potency than amlodipine, possibly because of disruption of a favourable interaction between the protonated amino group on the 2-substituentand the DHP receptor.Replacement of the 6-methyl substituent in amlodipine by alkoxyalkyl groups or electron-withdrawing groups is also detrimental to calcium antagonist activity. amlodipine / 1,4-dihydropyridine / structure activity relationship